Results 171 to 180 of about 4,995,094 (293)

Discovery of VU6052254: A Novel, Potent M₁ Positive Allosteric Modulator. [PDF]

ACS Chem Neurosci
Engers JL, Bungard JD, Presley CC, Zagol-Ikapitte I, Watson KJ, Chang S, O'Carroll C, Dey PM, Burstein ES, Dickerson JW, Thompson Gray A, Bubser M, Rook JM, Cho HP, Kramlinger VM, Boutaud O, Jones CK, Conn PJ, Engers DW, Lindsley CW.   +19 more
europepmc   +1 more source

Late INa as a Therapeutic Target: New Strategies, Computational Modelling, Drug Development, and Clinical Translation

Medicinal Research Reviews, EarlyView.
ABSTRACT The Nav1.5 channel, a major isoform of voltage‐gated sodium ion channel, is mainly found in ventricular cardiomyocytes, playing a key role in generating essential cardiac action potentials for normal heart rhythms. Mutations in Nav1.5 have been associated with severe heart conditions such as long QT syndrome, Brugada syndrome, cardiac ...
Arkapravo Chattopadhyay, Lynn C. Lunsonga, Peter E. Light, Khaled Barakat   +3 more
wiley   +1 more source

Discovery of VU6053371/BI03738809: A First-in-Class Selective and CNS-Penetrant mGlu₃ Positive Allosteric Modulator (PAM) with Efficacy in a Preclinical Cognition Model. [PDF]

ACS Chem Neurosci
Jones CA, Duncan RA, Gilliland KM, Reed CW, Haymer DH, Spearing PK, Capstick RA, Roland BP, Vinson P, Quitalig M, Baggeroer C, Billard NB, Dickerson JW, Xiang Z, Kramlinger VM, Boutaud O, Schlichtiger J, Jones CK, Niswender CM, Cho HP, Rook JL, Wotjak CT, Freiwald M, Giovannini R, Sommer H, Hobson S, Conn PJ, Melancon BJ, Lindsley CW.   +28 more
europepmc   +1 more source

Hsp90 Inhibition on the Western Blot: N‐Terminal Versus C‐Terminal Inhibitors in Breast Cancer

Medicinal Research Reviews, EarlyView.
ABSTRACT Heat shock protein 90 (Hsp90) is an established and clinically validated anticancer target. By regulating the folding and maturation of diverse client proteins, it is indirectly involved in carcinogenesis. Key breast cancer oncogenic drivers, including estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2, are ...
Jaka Dernovšek, Jernej Cingl, Urša Pečar Fonović, Tihomir Tomašič   +3 more
wiley   +1 more source

α6GABA_A receptor-selective positive allosteric modulator as a novel therapy for fibromyalgia: A proof-of-concept study in mice modeling chronic widespread musculoskeletal pain. [PDF]

Neurotherapeutics
Sant-Cassia M, Lee CH, Phani Babu Tiruveedhula VVN, Cook J, Chen CC, Chiou LC.   +5 more
europepmc   +1 more source

The FGF/FGFR System in the Biology and Therapeutic Landscape of Pediatric CNS Tumors

Medicinal Research Reviews, EarlyView.
ABSTRACT Central nervous system (CNS) tumors are the most common solid malignancies in children, comprising a highly heterogeneous group of neoplasms defined by distinct molecular alterations and clinical behaviors. Advances in molecular genetics have underscored the relevance of specific signaling pathways in driving pediatric tumorigenesis, among ...
Serena Filiberti, Camilla Tavani, Elena Somenza, Nicolas Tassone, Antonio d'Amati, Marta Turati, Roberto Ronca   +6 more
wiley   +1 more source

Navigating the Complexity: A Comprehensive Review of GSK‐3 Inhibition in Regenerative Medicine

Medicinal Research Reviews, EarlyView.
ABSTRACT Glycogen synthase kinase‐3 (GSK‐3) is a central regulator of numerous cellular signaling pathways, with critical roles in metabolism, proliferation, differentiation, and tissue regeneration. This review explores the multifaceted effects of pharmacological GSK‐3 inhibition across multiple body districts, focusing on its highly context‐dependent
Davide Schiroli, Alessia Merra, Chiara Marraccini, Lucia Merolle, Graziella Pellegrini, Eleonora Maurizi   +5 more
wiley   +1 more source

A positive allosteric modulator of the β1AR with antagonist activity for catecholaminergic polymorphic ventricular tachycardia. [PDF]

J Clin Invest
Grogan A, Perelli RM, Ahn S, Jiang H, Jyothidasan A, Sood D, You C, Israel DI, Shaginian A, Chen Q, Liu J, Wang J, Steyaert J, Kahsai AW, Landstrom AP, Lefkowitz RJ, Rockman HA.   +16 more
europepmc   +1 more source

Advancing Therapies for Mycobacterial Diseases: From Small Molecules to Host‐Directed Strategies

Medicinal Research Reviews, EarlyView.
ABSTRACT The global burden of multidrug‐resistant tuberculosis (MDR‐TB) and the rising incidence of nontuberculous mycobacterial (NTM) infections highlight the urgent need for innovative therapeutic strategies. Current treatments are prolonged, toxic, and increasingly compromised by resistance and limited diagnostic capacity.
Tânia Silva, Alessandra Aiello, Tonino Alonzi, M. Alice Carvalho, Vladimir Finger, Delia Goletti, Sven Hoffner, Yousra Kherabi, Jan Korabecny, Julia Kulczyńska, Agnieszka Kyzioł, Alicia Lacoma, Filomena Martins, Zorica Nanovic, Sepideh Hosseiniporgham, Martina Hrast Rambaher, Leonardo Antonio Sechi, Daria Smalchuk, Grażyna Stochel, Lydia Tabernero, Nancy L. Tateosian, Violeta Valcheva, Anamarija Zega, Mafalda Sarraguça   +23 more
wiley   +1 more source

An orally bioavailable MrgprX1-positive allosteric modulator alleviates certain neuropathic pain-related behaviors in humanized mice. [PDF]

Sci Transl Med
Uniyal A, Hin N, Zhang C, Xu Q, Huang Q, Berhane I, Thomas AG, Maragakis J, Gori S, Liu J, Zheng Q, Cui X, Peng Q, Wan J, Rais R, Slusher BS, Raja SN, Dong X, Tsukamoto T, Guan Y.   +19 more
europepmc   +1 more source